2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase

Histone Methyltransferase

Histone Methyltransferase

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Histone modifications play critical roles in regulating both global and stage-specific gene expression. Methylation on histones H3K4, H3K36 and H3K79 is generally associated with gene activation, whereas methylation on histones H3K9 and H3K27 is generally associated with gene repression. Histone lysine methylation is dynamically regulated by site-specific methyltransferases and demethylases. EZH2 (the catalytic subunit of PRC2) is responsible for the methylation of H3K27 in cells.

DOT1L is a histone H3 lysine 79 methyltransferase whose inhibition increases the yield of induced pluripotent stem cells (iPSCs). EPZ-5676 is a potent and selective DOT1L inhibitor.

Crucial to PRC2 activity, the histone methyltransferase enhancer of zeste homolog 2 (EZH2) tri-methylates lysine 27 of histone 3 (H3K27me3), leading to chromatin condensation and transcriptional repression.

Histone Methyltransferase Isoform Specific Products:

Histone Methyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161759
    MS152
    		Inhibitor 99.36%
    MS152 is an oral bioactive inhibitor of EHMT2/G9a. MS152 reactivats maternally silenced Prader-Willi syndrome (PWS) genes in brain and liver tissues of PWS mouse models.
    MS152
  • HY-15214
    CARM1-IN-3
    		Inhibitor 98.90%
    CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively.
    CARM1-IN-3
  • HY-160801
    HKYK-0030
    		Inhibitor 99.38%
    HKYK-0030 is an inhibitor for MTDH-SND1 protein-protein interaction. HKYK-0030 exhibits inhibitory activity against cancer metastasis.
    HKYK-0030
  • HY-155050
    PRMT5-IN-31
    		Inhibitor 99.25%
    PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min).
    PRMT5-IN-31
  • HY-134828
    AZ506
    		Inhibitor 99.74%
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
    AZ506
  • HY-152243
    YEATS4 binder-1
    YEATS4 binder-1(4e) is a potent and selective YEATS4 binder that binds to the KAc recognition site of the YEATS structural domain with a Ki value of 37 nM.
    YEATS4 binder-1
  • HY-170494
    AS-254s
    		Inhibitor 98.13%
    AS-254s is the inhibitor for absent, small, or homeotic-like 1 protein (ASH1L) with an IC50 of 94 nM (FP assay). AS-254s exhibits antiproliferative activity against MLL1-rearranged leukemic cells with GI50 <1 μM. AS-254s induces the differentiation of MLL1-r leukemic cell.
    AS-254s
  • HY-146999
    YM458
    		Inhibitor 99.16%
    YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
    YM458
  • HY-168035
    W4275
    		Inhibitor 98.93%
    W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research.
    W4275
  • HY-152236
    PRMT6-IN-3
    		Inhibitor 99.66%
    PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor with an IC50 value of 192 nM. PRMT6-IN-3 can induce apoptosis in cancer cells and has anticancer activity.
    PRMT6-IN-3
  • HY-142095
    NSD3-IN-3
    		Inhibitor 98.0%
    NSD3-IN-3 is a potent NSD3 inhibtor with an IC50 value of 1.86 μM. NSD3-IN-3 has anticancer activity and significantly inhibits the growth and proliferation of non-small cell lung cancer cell line H460.
    NSD3-IN-3
  • HY-P2254
    H3K27(Me3) (15-34)
    H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me).
    H3K27(Me3) (15-34)
  • HY-W011927R
    4,4'-Sulfonyldiphenol (Standard)
    		Agonist
    4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
    4,4'-Sulfonyldiphenol (Standard)
  • HY-128579
    DW14800
    		Inhibitor 99.63%
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
    DW14800
  • HY-100757
    CPUY074020
    		Inhibitor 98.56%
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
    CPUY074020
  • HY-112165
    PRMT5-IN-2
    		Inhibitor 98.68%
    PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3.
    PRMT5-IN-2
  • HY-162003A
    DCPT1061 hydrochloride
    		Inhibitor 99.88%
    DCPT1061 hydrochloride has a strong inhibitory effect on PRMT1, PRMT6, and PRMT8 in vitro, The epigenetic enzymes such as PRMT3, PRMT4 and PRMT5 had little inhibitory effect. DCPT1061 hydrochloride has antitumor effects.
    DCPT1061 hydrochloride
  • HY-157251A
    UNC8153
    		Degrader 99.13%
    UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2.
    UNC8153
  • HY-125244
    LEM-14-1189
    		Inhibitor 99.57%
    LEM-14-1189, a LEM-14 (HY-114340) derivative, is a NSDs inhibitor with IC50s of 418 μM (NSD1), 111 μM (NSD2), and 60 μM (NSD3), respectively. The NSDs, histone lysine methyltransferases (HMTases), are oncoproteins, drivers of a number of tumors. LEM-14-1189 can be used for multiple myeloma (MM) research.
    LEM-14-1189
  • HY-111213
    PRMT5-IN-20
    		Inhibitor 99.20%
    PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity.
    PRMT5-IN-20
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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